Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in Osteoporosis

Abstract

Bone-specific functionalization strategies on liposomes are promising approaches to delivering the drug in osteoporotic conditions. This approach delivers the drug to the bone surface specifically, reduces the dose and off-target effects of the drug, and thereby reduces the toxicity of the drug. The purpose of the current research work was to fabricate the bone-specific peptide conjugated pegylated nanoliposomes to deliver anabolic drug and its physicochemical evaluations. For this, a bone-specific peptide (SDSSD) was synthesized, and the synthesized peptide was conjugated with a linker (DSPE-PEG2000-COOH) to obtain a bone-specific conjugate (SDSSD-DSPE). Purified SDSSD-DSPE was characterized by HPLC, Maldi-TOF, NMR, and Scanning Electron Microscope/Energy Dispersive Spectroscopy (SEM/EDS). Further, peptide-conjugated and anabolic drug-encapsulated liposomes (SDSSD-LPs) were developed using the ethanol injection method and optimized by Central Composite Design (CCD) using a statistical approach. Optimized SDSSD-LPs were evaluated for their physicochemical properties, including surface morphology, particle size, zeta potential, in vitro drug release, and bone mineral binding potential. The obtained results from these studies demonstrated that SDSSD-DSPE conjugate and SDSSD-LPs were optimized successfully. The particle size, % EE, and zeta potential of SDSSD-LPs were observed to be 183.07 ± 0.85 nm, 66.72 ± 4.22%, and −25.03 ± 0.21 mV, respectively. SDSSD-LPs demonstrated a sustained drug release profile. Further, the in vitro bone mineral binding assay demonstrated that SDSSD-LPs deliver the drug to the bone surface specifically. These results suggested that SDSSD-LPs could be a potential targeting approach to deliver the anabolic drug in osteoporotic conditions.

Metal‐Organic Framework Based Mucoadhesive Nanodrugs for Multifunction Helicobacter Pylori Targeted Eradication, Inflammation Regulation and Gut Flora Protection

“…As depicted in Figure 1G, the Bi-MOF, which has been modified with CS-Se, demonstrated a positive charge and has the capability to bind to mucins that are negatively charged. [11] Collectively, these results over all demonstrated the successful preparation of Bi-MOF@CS-Se.…”

“…This interaction leads to its adherence to the gastric mucosa, ultimately enhancing gastric residence time. [11] The modification of chitosan with selenium elements further endows it with anti-inflammatory and antioxidative stress properties. [12] Therefore, functionalizing Bi-MOF with selenized chitosan (CS-Se) holds promise for achieving multi-effect therapy against H. pylori infection.…”

Construction Strategy of Functionalized Liposomes and Multidimensional Application

“…By incorporating nucleic acid drugs into the water compartment of liposomes, nucleic acid drugs can be effectively protected from nuclease-mediated degradation which improves cell uptake efficiency. [47] Han et al [2c] encapsulated siRNA in an aqueous core of anionic liposomes prepared with inorganic solvents by thin-film hydration. The results showed that anionic liposomes not only protected the integrity of siRNA in different physiological environments (at least 6 h in fetal bovine serum), but also effectively delivered siRNA into cells.…”

Collagen-Based Hydrogels for the Eye: A Comprehensive Review

“…In addition, the administration of a biodegradable matrix, including nanoparticles loaded with a potent drug, to the corneal surface has been found to be an appropriate option for treating inflammatory cases and for preventing postoperative infection in patients. Liposomes are termed a versatile drug delivery system [ 113 , 114 , 115 , 116 , 117 , 118 , 119 , 120 , 121 , 122 , 123 ]. Chang et al developed liposomes loaded with moxifloxacin (MFX) and dexamethasone (DEX) and mixed them with hydrogel-forming biodegradable materials (collagen/gelatin/alginate), i.e., CGA-Lipo-MFX/DEX, for prolonged ocular delivery [ 124 ] ( Figure 6 ).…”